Journal of Medicinal Chemistry p. 746 - 751 (1991)
Update date:2022-08-02
Topics:
Kukla, Michael J.
Breslin, Henry J.
Pauwels, Rudi
Fedde, Cynthia L.
Miranda, Milton
et al.
A series of 6-substituted 4,5,6,7-tetrahydro-5-methylimidazo<4,5,1-jk><1,4>benzodiazepin-2(1H)-ones (9) have been synthesized and tested for their ability to inhibit the replication of the HIV-1 virus in MT-4 cells.Two synthetic methods are described, one of which allows the synthesis of single enantiomers of the final products.A structure-activity study was done within the series of compounds to determine the optimum group for the 6-position substitution and to determine whether the activity was enantiospecific at the 5-position, which was substituted with a methyl group.The best analogue, 9jj, inhibited HIV-1 with an IC50 of 4 μM, which is comparable to the activity level of DDI, a 2',3'-dideoxynucleoside-type structure undergoing clinical trials as an anti-AIDS therapy.
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